نتایج جستجو برای: picolinamide

تعداد نتایج: 106  

2010
Thomas Scior José Antonio Guevara-García FJ Melendez Hassan H Abdallah Quoc-Tuan Do Philippe Bernard

Prior to its total synthesis, a new vanadium coordination compound, called TSAG0101, was computationally designed to inhibit the enzyme protein tyrosine phosphatase 1B (PTP1B). The PTP1B acts as a negative regulator of insulin signaling by blocking the active site where phosphate hydrolysis of the insulin receptor takes place. TSAG001, [V(V)O(2)(OH)(picolinamide)], was characterized by infrared...

2011
Jichun Zhang Jin Wu Jun Toyohara Yuko Fujita Hongxian Chen Kenji Hashimoto

Glycine transporter-1 (GlyT-1) in glial cells regulates extracellular levels of glycine, which acts as an obligatory co-agonist at the N-methyl-D-aspartate (NMDA) receptors in the brain. In the present study, we developed a novel radioligand, [³H]3-chloro-N-((S)-((R)-1-methylpiperidin-2-yl)(thiophen- 3-yl)methyl)-4- (trifluoromethyl)picolinamide ([³H]CHIBA-3007), for studying GlyT-1 in the brai...

Journal: :The Journal of pharmacology and experimental therapeutics 2016
Hilary Highfield Nickols Joannes P Yuh Karen J Gregory Ryan D Morrison Brittney S Bates Shaun R Stauffer Kyle A Emmitte Michael Bubser Weimin Peng Michael T Nedelcovych Analisa Thompson Xiaohui Lv Zixiu Xiang J Scott Daniels Colleen M Niswender Craig W Lindsley Carrie K Jones P Jeffrey Conn

Negative allosteric modulators (NAMs) of metabotropic glutamate receptor subtype 5 (mGlu5) have potential applications in the treatment of fragile X syndrome, levodopa-induced dyskinesia in Parkinson disease, Alzheimer disease, addiction, and anxiety; however, clinical and preclinical studies raise concerns that complete blockade of mGlu5 and inverse agonist activity of current mGlu5 NAMs contr...

2013
M. J. Noetzel K. J. Gregory P. N. Vinson J. T. Manka S. R. Stauffer C. W. Lindsley C. M. Niswender Z. Xiang P. J. Conn

Metabotropic glutamate receptor 5 (mGlu5) is a target for the treatment of central nervous system (CNS) disorders, such as schizophrenia and Alzheimer’s disease. Furthermore, mGlu5 has been shown to play an important role in hippocampal synaptic plasticity, specifically in long-term depression (LTD) and longterm potentiation (LTP), which is thought to be involved in cognition. Multiple mGlu5-po...

2015
Hilary Highfield Nickols Joannes P. Yuh Karen J. Gregory Ryan D. Morrison Brittney S. Bates Shaun R. Stauffer Kyle A. Emmitte Michael Bubser Weimin Peng Michael T. Nedelcovych Analisa Thompson Xiaohui Lv Zixiu Xiang J. Scott Daniels Colleen M. Niswender Craig W. Lindsley Carrie K. Jones Jeffrey Conn

Negative allosteric modulators (NAMs) of metabotropic glutamate receptor subtype 5 (mGlu5) have potential applications in the treatment of fragile X syndrome, levodopa-induced dyskinesia in Parkinson disease, Alzheimer disease, addiction, and anxiety; however, clinical and preclinical studies raise concerns that complete blockade of mGlu5 and inverse agonist activity of current mGlu5 NAMs contr...

2014
Palash Sanphui Geetha Bolla Ashwini Nangia Vladimir Chernyshev

Acemetacin (ACM) is a non-steroidal anti-inflammatory drug (NSAID), which causes reduced gastric damage compared with indomethacin. However, acemetacin has a tendency to form a less soluble hydrate in the aqueous medium. We noted difficulties in the preparation of cocrystals and salts of acemetacin by mechanochemical methods, because this drug tends to form a hydrate during any kind of solution...

Journal: :Molecular pharmacology 2013
M J Noetzel K J Gregory P N Vinson J T Manka S R Stauffer C W Lindsley C M Niswender Z Xiang P J Conn

Metabotropic glutamate receptor 5 (mGlu5) is a target for the treatment of central nervous system (CNS) disorders, such as schizophrenia and Alzheimer's disease. Furthermore, mGlu5 has been shown to play an important role in hippocampal synaptic plasticity, specifically in long-term depression (LTD) and long-term potentiation (LTP), which is thought to be involved in cognition. Multiple mGlu5-p...

Journal: :The Journal of pharmacology and experimental therapeutics 2012
Carrie K Jones Michael Bubser Analisa D Thompson Jonathan W Dickerson Nathalie Turle-Lorenzo Marianne Amalric Anna L Blobaum Thomas M Bridges Ryan D Morrison Satyawan Jadhav Darren W Engers Kimberly Italiano Jacob Bode J Scott Daniels Craig W Lindsley Corey R Hopkins P Jeffrey Conn Colleen M Niswender

Parkinson's disease (PD) is a debilitating neurodegenerative disorder associated with severe motor impairments caused by the loss of dopaminergic innervation of the striatum. Previous studies have demonstrated that positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGlu₄), including N-phenyl-7-(hydroxyimino) cyclopropa[b]chromen-1a-carboxamide, can produce antiparkinson...

Journal: :Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology 2011
Zhi-Xing Cao Ren-Lin Zheng Hong-Jun Lin Shi-Dong Luo Yan Zhou You-Zhi Xu Xiu-Xiu Zeng Zhao Wang Li-Na Zhou Yong-Qiu Mao Li Yang Yu-Quan Wei Luo-Ting Yu Sheng-Yong Yang Ying-Lan Zhao

Antagonizing angiogenesis-related receptor tyrosine kinase is a promising therapeutic strategy in oncology. In present study, we designed and synthesized a novel vascular endothelial growth factor receptor (VEGFR) inhibitor N-methyl-4-(4-(3-(trifluoromethyl) benzamido) phenoxy) picolinamide SKLB610 that potently suppresses human tumor angiogenesis. SKLB610 inhibited angiogenesis-related tyrosin...

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